N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides

Patent metadata

Field	Value
Publication number	US-9290485-B2
Application number	US-201113194009-A
Country	US
Kind code	B2
Filing date	Jul 29, 2011
Priority date	Aug 4, 2010
Publication date	Mar 22, 2016
Grant date	Mar 22, 2016

Abstract

The invention relates to compound of the formula I

in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

First claim

The invention claimed is:

1. A compound, or salt thereof, of Formula 1 A:

wherein
R 1 and R 3 are C 1-4 alkyl;
A is a ring system selected from

wherein the bond marked with the asterisk is attached to the carboxamide group and wherein each R 8 is hydrogen;
L is —C(R 10 ) 2 —; and each R 10 is hydrogen;
B is a quinolinyl, wherein the quinolinyl may be substituted once or more than once by R 12 ;
and wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen;
each R 12 independently is halogen; —X 2 —R 13 ;
X 2 is selected from bond; and
R 13 is C 1-6 alkyl; C 1-6 halogenalkyl.

2. A compound, or salt thereof, of claim 1
wherein
R 1 and R 3 are C 1-4 alkyl;
A is a ring system selected from

wherein the bond marked with the asterisk is attached to the carboxamide group and wherein each R 8 is hydrogen;
L is —C(R 10 ) 2 - ; and each R 10 is hydrogen;
B is a quinolin-2-yl, quinol-3-yl, quinol-6-yl, wherein the quinolinyl may be substituted once or more than once by R 12 ; and wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen;
each R 12 independently is halogen; —X 2 —R 13 ;
X 2 is selected from bond; and
R 13 is C 1-6 alkyl; C 1-6 halogenalkyl.

3. A compound, or salt thereof, of claim 1 selected from:
N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((2-methylquinolin-6-yl)methyl)-1H-1,2,3-triazole-4-carboxamide;
N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((7-methylquinolin-3-yl)methyl)-1H-1,2,3-triazole-4-carboxamide; and
N-((6-amino-2,4-dimethylpyridin-3-yl)methyl)-1-((7-chloroquinolin-2-yl)methyl)-1H-1,2,3-triazole-4-carboxamide.

4. A compound, or salt thereof, of claim 1 wherein the compound is

5. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 in free form or in pharmaceutically acceptable salt form and one or more pharmaceutically acceptable carriers.

Assignees

• Brandl Trixi
• Flohr Stefanie
• Kopec Sebastian
• Lachal Julie
• Markert Christian
• Namoto Kenji
• Nganga Perle
• Pirard Bernard
• Renatus Martin
• Sedrani Richard
• Zoller Thomas
• Novartis Ag

Inventors

• Brandl Trixi
• Flohr Stefanie
• Kopec Sebastian
• Lachal Julie
• Markert Christian
• Namoto Kenji
• Nganga Perle
• Pirard Bernard
• Renatus Martin
• Sedrani Richard
• Zoller Thomas

Classifications

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P7/10

  Antioedematous agents; Diuretics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/12

  Antihypertensives · CPC title